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Plural hetero atoms in the bicyclo ring system

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514277000 - Hetero ring is six-membered consisting of one nitrogen and five carbon atoms

514279000 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos

514299000 - Bicyclo ring system having the six-membered hetero ring as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514303000 Exactly three ring nitrogens in the bicyclo ring system 149
514301000 Ring sulfur in the bicyclo ring system 127
514302000 Ring oxygen in the bicyclo ring system 45
Entries
DocumentTitleDate
20080221149Novel 2-Heteroaryl Substituted Benzothiophenes and Benzofuranes 709 - The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below:09-11-2008
20120172391NAPHTHYRIDINONE ANALOGS AS MGLUR5 POSITIVE ALLOSTERIC MODULATORS - In one aspect, the invention relates to naphthyridinone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.07-05-2012
20080242694Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith - Provided herein are Heterocyclic Compounds having the following structure:10-02-2008
20100056563NOVEL 1.8-NAPHTHYRIDINE COMPOUNDS - The present invention relates to naphthyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.03-04-2010
201000630875-Amino-4-Hydroxy-7-(Imidazo [1,2-A] Pyridin-6-Ylmethyl)-8-Methyl-Nonamide Derivatives and Related Compounds as Renin Inhibitors for the Treatment of Hypertension - Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH03-11-2010
20090023769Organic Compounds - Compounds of formula I01-22-2009
201101959913-AMINOIMIDAZO [1,2-A] PYRIDINE DERIVATIVES AS SGLT INHIBITORS - Novel compounds of the formula I, in which X, Y, R, R′, R08-11-2011
20130085153COMBINATION OF AN IAP INHIBITOR AND A TAXANE FOR THE TREATMENT OF A PROLIFERATIVE DISEASE - The invention provides a pharmaceutical combination comprising: 04-04-2013
20130210858SULFAMOYL BENZOIC ACID HETEROBICYCLIC DERIVATIVES AS TRPM8 ANTAGONISTS - The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.08-15-2013
20130210857Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.08-15-2013
20130210856COMPOSITIONS AND METHODS FOR TREATING SLEEP DISORDERS - The present invention provides liquid dosage forms for treating narcolepsy. The liquid dosage form includes zolpidem or a pharmaceutically acceptable salt thereof, a carbonate salt, a metal oxide, and a borate salt. The present invention also provides methods for treating somnambulism. The methods include administering an emulsion that includes zolpidem, a bicarbonate salt, a citrate salt, and a phosphate salt.08-15-2013
20120245199[4 [4-(AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL- )-METHANONES AND SYNTHESIS THEREOF - The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase.09-27-2012
20120245198COMPOUNDS AND COMPOSITIONS FOR TREATMENT OF CANCER - Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions.09-27-2012
20120245197PHARMACEUTICAL COMPOSITION CONTAINING TOSUFLOXACIN OR SALT THEREOF - A pharmaceutical composition containing tosufloxacin or a salt thereof, which is excellent in stability and preservative effect and contamination preventing effect is provided. A pharmaceutical composition containing tosufloxacin or a salt thereof, a metal compound comprising aluminum, borax, an alkali metal chloride and a preservative is excellent in stability and preservative effect and contamination preventing effect, and useful especially as eye drops, nasal drops and ear drops.09-27-2012
20130079365NEW BICYCLIC DIHYDROQUINOLINE-2-ONE DERIVATIVES - The invention provides novel compounds having the general formula (I)03-28-2013
20090143421USE OF 2-BENZOYL-IMIDAZOPYRIDINES IN THERAPEUTICS - The present invention is related to the use of a compound of formula (I):06-04-2009
20130035353DRUGS FOR THE TREATMENT OF SARCOGLYCANOPATHIES - Inhibitors of the endoplasmic reticulum associated degradation (ERAD) pathway, particularly inhibitors of mannosidase I, are used for the preparation of a medicinal product intended to treat sarcoglycanopathies.02-07-2013
20130035354ARYL PYRIDINE AS ALDOSTERONE SYNTHASE INHIBITORS - The present invention provides a compound of formula I;02-07-2013
20090005411Combinations of Organic Compounds - The invention provides a pharmaceutical combination comprising: 01-01-2009
201300409847-(lH-PYRAZOL-4-YL)-1,6-NAPHTHYRIDINE COMPOUNDS AS SYK INHIBITORS - The present invention relates to a compound of formula (I):02-14-2013
20130040983RAF KINASE INHIBITORS - Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.02-14-2013
20120208837SUBSTITUTED AZAINDOLES - This invention relates to novel substituted azaindoles and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound showing selective inhibitory activity of oncogenic B-Raf08-16-2012
20090163535Substituted Heteroarylalkanoic Acids - Disclosed are substituted heteroarylalkanoic acids of the following formula D-A-C(O)R′, where D, A, and R′ are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.06-25-2009
20100041693INDOLYLMALEIMIDE DERIVATIVES - A compound of formula (I)02-18-2010
20100041694AGRICULTURAL COMPOSITION FOR CONTROLLING OR PREVENTING PLANT DISEASES CAUSED BY PLANT PATHOGENIC MICROBES - An agricultural composition comprising an amide compound represented by the following formula (I),02-18-2010
20100105721IMIDAZO[1,2-a]PYRIDINE DERIVATIVES: PREPARATION AND PHARMACEUTICAL APPLICATIONS - The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC).04-29-2010
20100105720PREPARATION AND UTILITY OF SUBSTITUTED IMIDAZOPYRIDINE COMPOUNDS WITH HYPNOTIC EFFECTS - The present disclosure is directed to modulators of GABA04-29-2010
20100137355NITROGENOUS HETEROCYCLIC COMPOUNDS, PREPARATION THEREOF AND USE THEREOF AS ANTIBACTERIAL MEDICAMENTS - The invention concerns nitrogenated heterocyclic compounds, their preparation and use as antibacterial drugs, compounds of general formula (I)06-03-2010
20100093784NOVEL HETEROCYCLIC NITROGENOUS COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL MEDICAMENTS - The invention relates to nitrogenous heterocyclic compounds of formula04-15-2010
20090042927Salts, Prodrugs and Polymorphs of Fab I Inhibitors - In part, the present invention is directed to antibacterial compounds and salts thereof.02-12-2009
20090042928Modulators of muscarinic receptors - The modulator compounds described herein modulate muscarinic receptors and are useful for treating muscarinic receptor mediated diseases.02-12-2009
20130090351ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I04-11-2013
20090318492INDOLE COMPOUNDS HAVING C4-ACIDIC SUBSTITUENTS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS - Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.12-24-2009
20090312365Certain Chemical Entities, Compositions, and Methods - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.12-17-2009
20100130539IMIDAZOPYRIDINE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein Q, X05-27-2010
20130090352TETRAHYDROQUINOLINE AMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to tetrahydroquinoline amide compounds of formula (I) (Formula should be inserted here) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.04-11-2013
20090306128PHARMACEUTICAL COMPOSITIONS CONTAINING A FLUOROQUINOLONE ANTIBIOTIC DRUG - Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions.12-10-2009
20090306127Certain Chemical Entities, Compositions and Methods - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.12-10-2009
20090306126Indole Derivatives - The invention concerns indole derivatives of Formula I12-10-2009
200903061243-(INDOLYL)-4-ARYLMALEIMIDE DERIVATIVES AND THEIR USE AS ANGIOGENESIS INHIBITORS - The present invention relates to a compound of formula (I) wherein R12-10-2009
20090306123Bicyclononene derivaties - The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.12-10-2009
20130059880MOXIFLOXACIN HYDROCHLORIDE COMPOUNDS AND INTERMEDIATES AND METHODS FOR MAKING SAME - Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.03-07-2013
20130059881COMPOSITIONS AND METHODS FOR TREATING VIRAL DISEASES - Substituted perhydro pyrrolopyridines and methods for their use in the treatment of viral diseases including hepatitis C viral infections are described herein.03-07-2013
20090291978Enzyme Inhibitors - Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R11-26-2009
200902704441,7-Naphthyridines - There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof,10-29-2009
20130065917SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.03-14-2013
20120115899NAPHTHYRIDIN-2 (1 H)-ONE COMPOUNDS USEFUL AS ANTIBACTERIALS - Compounds of Formula (I),05-10-2012
20090215816Imidazo(1,2-a)Pyridine Derivatives Useful as Peptide Deformylase (PDF) Inhibitors - The present invention relates to compounds of formula (I). These compounds are a novel type of peptide deformylase (PDF) inhibitors, and are therefore of great interest especially as new antibiotics.08-27-2009
200901434202-BENZOYLIMIDAZOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present invention is related to a compound of formula (I)06-04-2009
20120238598DERIVATIVES OF 7 ALKYNYL-1,8 NAPHTHYRIDONES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The disclosure relates to method of treating a disease in which VEGFR-3 is involved, comprising administering a therapeutically effective amount of a compound of the formula09-20-2012
20120238597Inhibiting EPH B-3 Kinase - EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke.09-20-2012
20130165475DEUTERIUM-ENRICHED HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS - The present invention provides deuterium-enriched heteroaryl-containing urea compounds (I) and use of the same for treating conditions mediated by protein kinase such as 06-27-2013
20080262026Therapeutic Agents 684 - Certain 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, methods for their therapeutic use and pharmaceutical compositions containing them are described.10-23-2008
20080293761Pyrrolopyridine-2-Carboxylic Acid Amide Derivative Useful as Inhibitor of Glycogen Phosphorylase - The present invention is directed to a novel form of a pyrrolopyridine-2-carboxylic acid amide of formula (I), which is an inhibitor of glycogen phosphorylase, compositions containing it and their use in therapy. The invention is also directed to processes for production of the novel form, novel intermediates used in said processes and processes for the production of said intermediates.11-27-2008
20130165473Azaquinolinone Derivatives and Uses Thereof - The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.06-27-2013
20130165474COMPOUNDS THAT INHIBIT TAU PHOSPHORYLATION - The present invention provides methods and compositions for enhancing working memory impaired in a tau pathological condition associated with AD or Down's syndrome.06-27-2013
20090170893NOVEL HYDRATE FORM - The present invention relates to a novel hydrate form of moxifloxacin monohydrochloride, processes for preparing the form, pharmaceutical compositions comprising the form and uses of the form and compositions.07-02-2009
20120289541METHODS AND COMPOSITIONS FOR APPLYING MOXIFLOXACIN TO THE EAR - Methods and materials useful for applying moxifloxacin to the ear are described. The methods involve delivering a composition that contains at least one viscogenic agent and moxifloxacin or a salt thereof to the epidermal surface of the tympanic membrane via the ear canal. The composition is delivered to the tympanic membrane in a flowable form and, after delivery to the tympanic membrane, becomes sufficiently viscous such that the moxifloxacin is localized against the tympanic membrane. Such compositions can be used to prophylactically and/or therapeutically treat middle and inner ear conditions, including otitis media.11-15-2012
20110136855GEMIFLOXACIN PROCESS AND POLYMORPHS - The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.06-09-2011
20090069368FGF-RECEPTOR AGONIST DIMERIC COMPOUNDS - FGF receptor agonist compounds corresponding to the general formula: M1-L-M2 are disclosed in which M1 and M2, which may be identical or different, each represent, independently of one another, a monomer unit M, and L represents a linker group, wherein the monomer unit is of the general formula I.03-12-2009
20110112136NOVEL PROCESS FOR THE MANUFACTURE OF PHARMACEUTICAL PREPARATIONS - The present invention is related to an improved method for the manufacture of Micro-precipitated Bulk Powder (MBP) containing the active pharmaceutical ingredient Propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-05-12-2011
20100152229Process for the Synthesis of Moxifloxacin Hydrochloride - A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II):06-17-2010
20090286826PHARMACEUTICAL COMPOSITIONS HAVING CARBOXYVINYL POLYMER AND POVIDONE POLYMER - The present invention is directed to pharmaceutical compositions, such as ophthalmic gels. The compositions typically include a carboxyvinyl polymer. A povidone polymer is also typically included to stabilize the carboxyvinyl polymer against agents or ingredients (e.g., therapeutic agent) that can otherwise cause instability to the carboxyvinyl polymer.11-19-2009
20100137356AZAINDOLE-INDOLE COUPLED DERIVATIVES, PREPARATION METHODS AND USES THEREOF - A novel class of azaindole-indole coupled derivatives, their preparation methods, pharmaceutical compositions containing the same and the uses thereof. The common structural feature of these derivatives is that they are coupled by azaindole and indole bi-molecule at different positions, forming extended pi-conjugated systems. Such derivatives inhibited cell growth and proliferation by various mechanisms. The present compounds have improved solubility, increased bioavailability, and thus have enhanced drug actions, and reduced medical dosages and undesired responses.06-03-2010
20100035919COMPOUNDS USEFUL AS INHIBITORS OF PROTEIN KINASES - Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof,02-11-2010
20100035917PYRROLO[2,3-B]PYRIDIN-4-YL-BENZENESULFONAMIDE COMPOUNDS AS 1KK2 INHIBITORS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to Formula (1) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular 1KK2 activity.02-11-2010
20100010036DRUGS FOR THE TREATMENT OF SARCOGLYCANOPATHIES - Inhibitors of the endoplasmic reticulum associated degradation (ERAD) pathway, particularly inhibitors of mannosidase I, are used for the preparation of a medicinal product intended to treat sarcoglycanopathies.01-14-2010
20080293760Gemifloxacin Process and Polymorphs - The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.11-27-2008
20100113505AMINO-NAPHTHYRIDINE DERIVATIVES - The present invention relates to new compounds having an amino-naphthyridine group. In particular, the present invention relates to new compounds, its stereoisomers and pharmaceutically acceptable salts or solvates thereof having a first unit (moiety) selected from the group of a phenyl derivative, a biphenyl derivative or a diphenyl alkane derivative and at least one amino-naphthyridine group linked with the first unit via a linking group. In specific embodiments, the present invention relates to compounds having a phenyl derivative unit and three amino-naphthyridine groups bound to the phenyl derivative unit via a linking group as well as salts or solvates thereof, in particular, pharmaceutically acceptable salts or solvates thereof. Further, the present invention relates to pharmaceutical compositions comprising said compounds. The compounds are particularly useful for treating or preventing infections, like viral infections.05-06-2010
20080312270COMPOUNDS AND METHODS USEFUL FOR TREATING ASTHMA AND ALLERGIC INFLAMMATION - Compounds, compositions and methods that are useful in the treatment of inflammatory and immune-related diseases and conditions are provided herein. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.12-18-2008
20090149494THERAPEUTIC USE OF IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES - The present invention is related to the use of a compound of formula (I):06-11-2009
20090149493INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R06-11-2009
20110039879METHODS FOR INCREASING WHITE BLOOD CELLS - The present invention relates to methods and compounds useful for increasing white blood cell levels in blood and bone marrow. Methods and compounds for increasing hematopoietic progenitor cells are also provided.02-17-2011
20090156631Controlled Release Compositions Containing Zolpidem - The present invention relates to controlled release compositions of Zolpidem or pharmaceutically acceptable salts thereof adapted to release Zolpidem over a predetermined time period, according to a monophasic and/or a biphasic profile of dissolution. The present invention also relates to monolithic matrix based formulations of Zolpidem or pharmaceutically acceptable salts thereof.06-18-2009
20120065225HETEROARYL PYRROLIDINYL AND PIPERIDINYL KETONE DERIVATIVES AND USES THEREOF - Compounds of the formula:03-15-2012
20100267763Method of Decreasing Pro-ADAM10 Secretase and/or Beta Secretase Levels - The present invention provides a method of decreasing the level of pro-ADAM10 and/or BACE protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof.10-21-2010
20130217719Combination of Organic Compounds - The invention provides a pharmaceutical combination comprising: 08-22-2013
20100249178COMPOSITIONS AND METHODS FOR TREATING MIDDLE-OF-THE-NIGHT INSOMNIA - The present invention provides compositions having a therapeutically effective amount of zolpidem, carbonate buffer, bicarbonate buffer, and a mixture comprising large and fine particles of silicon dioxide. Compositions having a therapeutically effective amount of zolpidem, carbonate buffer, bicarbonate buffer, and sodium stearyl fumarate are also described.09-30-2010
20100249177COMPOSITIONS AND METHODS FOR TREATING MIDDLE-OF-THE-NIGHT INSOMNIA - The present invention provides compositions for treating middle-of-the-night insomnia without residual sedative effects upon awakening by administering low doses (about 5 mg or less) of zolpidem or a salt thereof.09-30-2010
20100249176HETEROCYCLE AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS - The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.09-30-2010
20100120838COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I):05-13-2010
20090082390PIPERIDINE COMPOUNDS FOR USE AS OREXIN RECEPTOR ANTAGONIST - This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.03-26-2009
20130190349THERAPEUTIC COMPOSITIONS FOR INTRANASAL ADMINISTRATION OF ZOLPIDEM - The invention provides sprayable aqueous compositions containing zolpidem or single stereoisomer, mixtures of stereoisomers, pharmaceutically acceptable salts or prodrugs thereof, a solubilizing agent, a water soluble polymer with bioadhesive property. When administered intranasally using a spray device, zolpidem is rapidly absorbed with prolonged intranasal residence time and improved bioavailability. The compositions can be applied for the treatment of insomnia-related disorders such as difficulties with sleep initiation or middle of the night awakenings.07-25-2013
20100125087NEW COMPOUNDS 575 - The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.05-20-2010
20080207677Napthyridine Compounds As Rock Inhibitors - The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis.08-28-2008
200802076807-Azaindoles, their use as inhibitors of phosphodiesterase 4, and a method for synthesizing them - 7-azaindoles inhibit phosphodiesterase 4 (PDE4). Methods for preparing these compounds and methods of treating arthritis and other conditions with the compounds are also provided.08-28-2008
20080207679Glutathione peroxidase mimetics for the treatment of dermatoses - This invention relates to compositions and methods for the treatment of dermatological conditions with a glutathione peroxidase mimetic.08-28-2008
20080312269Therapeutic Agents - The present invention relates to 4,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one and 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.12-18-2008
20090298865Derivatives of pyrrolopyridine-2-carboxamides, preparation thereof and therapeutic application thereof - The invention relates to compounds of formula (I):12-03-2009
20110172265Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors - The present invention relates to fused pyrrolidino-cyclopropane derivatives according to formulae (I) to (IV) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-β-HSD-1) and the use of such compounds for the treatment and/or prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.07-14-2011
200803061061-HETEROCYCLYLALKYL-3-SULFONYLAZAINDOLE OR -AZAINDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.12-11-2008
20080207678VIRAL INHIBITORS - Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A),08-28-2008
20130217720IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR 2 MODULATORS - The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2).08-22-2013
20130217721COMPOSITIONS AND METHODS FOR DETECTION AND TREATMENT OF B-RAF INHIBITOR-RESISTANT MELANOMAS - Specific, targetable molecules mediating acquired resistance of B-RAF-mutant melanomas to a B-RAF inhibitor, thereby providing materials and methods for the treatment and detection of B-RAF inhibitor resistant cancers, such as melanoma. A method of identifying a patient to be treated with an alternative to B-RAF inhibitor therapy is described. Also described is a method of treating a patient having cancer. The patient is administered a MEK inhibitor, optionally in conjunction with vemurafenib therapy, or an inhibitor of the MAPK pathway (RAF, MEK, ERK) in conjunction with an inhibitor of the RTK-PI3K-AKT-mTOR pathway.08-22-2013
20090005410N-(2-(HETARYL)ARYL) ARYLSULFONAMIDES AND N-(2-(HETARYL) HETARYL ARYLSULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.01-01-2009
20080280947ANTI-INSOMNIA COMPOSITIONS AND METHODS - Compositions of zolpidem, and methods for their manufacture and use for treating insomnia. The compositions are formulated as oral sprays for transmucosal absorption of zolpidem. The methods of treatment in some cases involve night-time dosing administration to achieve therapeutic zolpidem blood levels within 20 minutes or less, tapering off to less than 20 ng/ml within less than five hours, in some cases less than four hours, post dosing.11-13-2008
20120295934New Hexahydrocyclopentapyrrolone, Hexahydropyrrolopyrrolone, Octahydropyrrolopyridinone and Octahydropyridinone Compounds - The invention provides novel compounds having the general formula (I)11-22-2012
20090264459Organic Compounds - Compounds of formula (I) in free or a pharmaceutically acceptable salt form, wherein X10-22-2009
20080269277Pyrrolopyridine-2-Carboxylic Acid Hydrazides - Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth.10-30-2008
20090005409Pyrrolo[3,2-C] Pyrdine Derivatives and Processes for the Preparation Thereof - The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect.01-01-2009
20090118322Agent for repairing corneal sensitivity containing amide compound - The amide compound of the formula (I) [each symbol is as defined in the description] has a promoting action on neuritogenesis of trigeminal nerve cells, and the compound is useful as a corneal neuritogenesis promoter, an agent for recovering corneal sensitivity by promotion of corneal neuritogenesis, and an agent for treating dry eye.05-07-2009
20090197909Bis-Heterocyclic Imidazolyl Compounds - The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R08-06-2009
20110144149GEMIFLOXACIN PROCESS AND POLYMORPHS - The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.06-16-2011
20090054478AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES - The present invention relates to azolopyridin-3-one derivatives of the general formula I with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances.02-26-2009
200900544774-thio substituted quinoline and naphthyridine compounds - The present invention relates to 4-thio substituted quinoline and naphthyridine derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 4-thio substituted quinoline or naphthyridine derivative.02-26-2009
20120289540KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES - The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.11-15-2012
20110224250ISOQUINOLINE DERIVATIVE, AND PDE INHIBITOR COMPRISING SAME AS ACTIVE INGREDIENT - The present invention provides a novel isoquinoline derivative which is useful as a pharmaceutical agent having a phosphodiesterase inhibitory activity.09-15-2011
20110224248AZAQUINOLONES THAT INHIBIT PROLYL HYDROXYLASE - Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure:09-15-2011
20090105297Compounds Modulating C-Kit Activity - Compounds with 7-azaindole core structure with activity toward the receptor protein tyrosine kinase c-kit, compositions useful for treatment c-kit-mediate diseases or conditions, and methods of use thereof, are provided. Further provided are methods of c-kit ligand identification and design.04-23-2009
20080262027Novel Chemical Compounds - This invention relates to newly identified compounds for inhibiting YAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of YAK3 proteins.10-23-2008
20080262025Processes for the Preparation of Zolpidem and its Hemitartrate - The invention relates to the preparation of a non-hygroscopic polymorphic form of zolpidem hemitartrate, designated as Form I, and pharmaceutical compositions including it. The invention also relates to use of the compositions for treating anxiety, sleep disorders and convulsions. The invention also relates to a process for the preparation of zolpidem or pharmaceutically acceptable salts thereof by condensing 3-bromo-N,N-dimethyl-4-oxo-4-p-tolyl-butyramide with 2-amino-5-methylpyridine in a polar aprotic solvent.10-23-2008
20090093515Substituted pyrroline kinase inhibitors - The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.04-09-2009
20120077840HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS - The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.03-29-2012
20090209573COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.08-20-2009
20090209574FLUOROQUINOLONE DERIVATIVES FOR OPHTHALMIC APPLICATIONS - The present invention relates to fluoroquinolone derivatives having enhanced ocular penetration characteristics and/or antimicrobial activity, and to compositions comprising such derivatives. The derivatives and compositions are particularly well suited for treating ophthalmic bacterial infections. The present invention more particularly relates to the discovery that a 2-methyl substitution on a diazabicyclo group attached to a fluoroquinolone ring system produces improved permeability characteristics, and that a 5-amino substitution on a fluoroquinolone ring system results in improved anti-microbial activity.08-20-2009
20090209575Method for treating neuropathic pain and associated syndromes - The present invention is directed to the use of ibudilast for treating neuropathic pain.08-20-2009
200902537352-ARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention is related to a compound of formula (I)10-08-2009
20090221629Method for antagonizing MIF activity - Methods of antagonizing MIF activity using ibudilast are described. Also described are methods of screening for MIF antagonists. These agents can be used for treating addictions, including drug and behavioral addictions, as well as for treating neuropathic pain.09-03-2009
20090253736AZAINDOLE DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.10-08-2009
20100035918Imidazolone Compounds and Methods of Making and Using the Same - In one aspect, the invention features a compound of the general Formula (I). Compounds of Formula (I) possess high affinity for Alk 5 and/or AIk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.02-11-2010
20100160369S1P1 Agonists and Methods of Making And Using - The invention is directed to Compounds of Formula I:06-24-2010
20100261751METHOD FOR DETERMINING ONE OF THE TWO HUMAN IMMUNODEFICIENCY VIRUS (HIV) INTEGRASE ENZYMATIC ACTIVITIES - The invention concerns a method for determining one of the two Human Immunodeficiency Virus (HIV) integrase enzymatic activities, in particular 3′-end processing, in an in vitro assay.10-14-2010
20090048285Pyrrolopyridines Useful in the Treatment of Inflammation - There is provided compounds of formula (I), wherein X02-19-2009
20100173932SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).07-08-2010
201001977246.5 -PYRROLOPIPERIDINE TACHYKININ RECEPTOR ANTAGONISTS - The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.08-05-2010
20100261750Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.10-14-2010
20100184800Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.07-22-2010
20090318493Aryl pyrrolidinyl and piperidinyl ketone derivatives and uses thereof - Aryl and heteroaryl ketone compounds substituted with pyrrolidines and piperidines, that modulate serotonin norepinephrine and/or dopamine neurotransmission. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.12-24-2009
20100227880CHEMICAL COMPOUNDS - The present invention provides compounds of formula (I):09-09-2010
20100240695STABILIZED ZOLPIDEM PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compositions for buccal delivery of zolpidem comprising an effective amount of zolpidem and a carbonate and bicarbonate buffer system in an amount sufficient to raise the pH of saliva to at least 8.5, and wherein the carbonate forms a coating on the bicarbonate wherein the amount of carbonate coating is at least 30% (w/w) of the total buffer amount are described. Pharmaceutical compositions for buccal delivery of zolpidem comprising an effective amount of zolpidem and a binary buffer system of carbonate and bicarbonate, wherein the carbonate and bicarbonate are co-located in a single particle, wherein the bicarbonate is coated with the carbonate, and wherein the amount of carbonate coating is at least 30% (w/w) of the binary buffer system are also described.09-23-2010
20100240694SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.09-23-2010
20100144781METHODS OF TREATING PSYCHOSIS AND SCHIZOPHRENIA BASED ON POLYMORPHISMS IN THE ERBB4 GENE - The present application is directed to the use of genetic polymorphism in the ErbB4 gene to predict whether a patient is likely to respond to psychotic medication Paliperidone. The polymorphism in the ErbB4 gene is also used to predict whether a patient is likely to display placebo effect among patients in need of psychotic treatment. A method of treating patients with antipsychotic medication Paliperidone using the polymorphism in the ErbB4 gene and a kit of are also provided.06-10-2010
201002278811,7-NAPHTHYRIDINE DERIVATIVES AS P38 MAP KINASE INHIBITORS - New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.09-09-2010
20090076066DEUTERIUM-ENRICHED ZOLPIDEM - The present application describes deuterium-enriched zolpidem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090076065DEUTERIUM-ENRICHED MK-0812 - The present application describes deuterium-enriched MK-0812, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20100144782DERIVATIVES OF 7-ALKYNYL-1,8-NAPHTHYRIDONES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The disclosure relates to compounds of formula (I):06-10-2010
20130217718TREATMENT OF PROGRESSIVE NEURODEGERATIVE DISEASE WITH IBUDILAST - Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).08-22-2013
20100081683NICOTINIC ACETYLCHOLINE RECEPTOR SUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).04-01-2010
20090239896AZAINDOLE COMPOUNDS AND USE THEREOF AS PHOSPHOLIPASE-A2 INHIBITORS - Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject. The compounds include azaindoles of the formula below [insert FIG. 09-24-2009
20130137715Pharmaceutical Compositions Containing A Fluoroquinolone Antibiotic Drug - Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions.05-30-2013
20090036481Novel Azaindole Inhibitors of Mtp and Apob - The present invention relates to 7-azaindole-based compounds, to processes for the preparation thereof, to pharmaceutical compositions comprising them, and to the use thereof in the preparation of medicaments that are useful as inhibitors of MTP and of ApoB secretion.02-05-2009
20130143912SUBLINGUAL ZOLPIDEM FORMULATIONS - The present disclosure provides pharmaceutical compositions for the delivery of a hypnotic agent across the oral mucosa. In particular, the compositions devoid of buffer and in the presence of alkaline oxides capable of raising the pH of saliva to a pH greater than about 7.0 thereby facilitate the substantially complete conversion of the hypnotic agent from its ionized to its un-ionized form. As a result, the dose of hypnotic agent is rapidly and efficiently absorbed by the oral mucosa with surprisingly low inter-subject variability. Furthermore, delivery of the hypnotic agent across the oral mucosa advantageously bypasses hepatic first pass metabolism of the drug and avoids enzymatic degradation of the drug within the gastrointestinal tract. Methods for using the compositions of the present invention for treating sleep disorders such as insomnia are also provided.06-06-2013
20110021556PYRROLIDINYL DERIVATIVES AND USES THEREOF - The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.01-27-2011
20110212990NOVEL POLYMORPH OF MOXIFLOXACIN HYDROCHLORIDE - The present invention relates to novel polymorph of moxifloxacin hydrochloride, processes for its preparation and to pharmaceutical compositions containing it. Thus, for example moxifloxacin hydrochloride is suspended in methanol and water and the p09-01-2011
20110039882PHOSPHODIESTERASE 10A INHIBITOR - A phosphodiesterase 10A inhibitor serving as an effective prophylactic or therapeutic agent for Parkinson's disease, Huntington's disease, Alzheimer's disease, and schizophrenia.02-17-2011
20110245290Alternative Forms of the Phosphodiesterase-4 Inhibitor N-Cyclopropyl-1--4-Oxo-1,4-Dihydro-1,8-Naphthyridine-3-Carboxyamide - The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below:10-06-2011
20110028511PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS - According to the present invention there are provided novel processes for the manufacture of the compound of formula 102-03-2011
20110039878METHODS FOR REDUCING BLOOD PRESSURE - The present invention provides methods and medicaments for reducing blood pressure. Methods and medicaments for treating or preventing hypertension are also provided.02-17-2011
20110039881COMPOSITIONS AND METHODS FOR TREATING MIDDLE-OF-THE-NIGHT INSOMNIA - The present invention provides compositions and methods for treating middle-of-the-night insomnia without residual sedative effects upon awakening by dosing an amount of zolpidem or a salt thereof to a subject who awakens from sleep and desires to resume sleep for less than 5 hours. The step of dosing is performed after the subject awakens from sleep and the amount permits the subject to awaken at a time about four hours after dosing without residual sedative effects.02-17-2011
20110112135Imidazo [1,2-A] Pyridine Compounds - This invention relates generally to imidazo[1,2-a]pyridine-based modulators of Liver X receptors (LXRs) having formula (I) and related methods:05-12-2011
20110086876STABLE SNS-595 COMPOSITIONS AND METHODS OF PREPARATION - Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.04-14-2011
20100029708COMPOUNDS AND COMPOSITIONS FOR TREATMENT OF CANCER - Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions.02-04-2010
20090312366NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.12-17-2009
20100069430PYRROLO[2,3-C]PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides novel pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect.03-18-2010
20090023770Novel 1,2,3-Substituted Indolizine Derivatives, Inhibitors of FGFs, Method for Preparing Them and Pharmaceutical Compositions Containing Them - The present invention relates to novel 1,2,3-substituted indolizine derivative which are inhibitors of fibroblast growth factors, to methods or preparing such derivatives, to pharmaceutical compositions comprising such derivatives, and to methods of treatment comprising such derivatives.01-22-2009
20100249175Dicationic compounds which selectively recognize G-quadruplex DNA - Dicationic compounds that are highly selective for binding G-quadruplex DNA are described. Several compounds exhibit groove binding toward G-quadruplex DNA and in vitro and in vivo activity versus 09-30-2010
20100130538BICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula05-27-2010
20110082169Stable SNS-595 Compositions and Methods of Preparation - Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.04-07-2011
20110152312ANTIPARISITIC DIHYDROAZOLE COMPOUNDS AND COMPOSITIONS COMPRISING SAME - The present invention relates to novel dihydroazole of formula (I) and salts thereof:06-23-2011
201002800638-ANILINOIMIDAZOPYRIDINES AND THEIR USE AS ANTI-CANCER AND/OR ANTI-INFLAMMATORY AGENTS - The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.11-04-2010
20100234417THYROTROPIN RELEASING HORMONE RECEPTOR-OREXIN RECEPTOR HETERO-DIMERS/-OLIGOMERS - A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.09-16-2010
20110212991Diagnostic Test for Susceptibility to B-RAF Kinase Inhibitors - The present invention provides methods and reagents for the detection of a mutation in BRAF and methods of selecting, patients for treatment if a B-Raf kinase inhibitor, such as a selective B-Raf kinase inhibitor.09-01-2011
20100035920SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE - The present invention is directed to substituted pyrazolo[1,5-a]pyridines and related methods for their synthesis and use.02-11-2010
20110257222COMPOUNDS AND METHODS FOR THE TREATMENT OF PAIN AND OTHER DISEASES - The present invention relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of MMP inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP inhibitors for the treatment of pain and other diseases such as cancer. Additionally, the present invention relates to methods for treating pain in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.10-20-2011
20080255182Certain chemical entities, compositions, and methods - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.10-16-2008
20110003845SUBSTITUTED AZABICYCLIC COMPOUNDS AND THE USE THEREOF - The present application relates to novel substituted pyrrolopyridine, pyrazolopyridine and isoxazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.01-06-2011
20110028512BIS-HETEROCYCLIC IMIDAZOLYL COMPOUNDS - Heterocyclic compounds of the general formula (I) are provided in which R, R02-03-2011
20110028513METHOD FOR TREATING NEUROLOGICAL DISORDERS WITH IMIDAZOLIUM AND IMIDAZOLINIUM COMPOUNDS - There is presently provided methods for delivering a neuroprotective agent to a neural cell. The methods comprise contacting a neural cell with an imidazolium or imidazolinium compound as described herein, including an imidazolium or imidazolinium salt.02-03-2011
20110028510Compositions, Methods, and Kits for Treating Influenza Viral Infections - The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infection caused by an influenza virus).02-03-2011
20100286190CERTAIN SUBSTITUTED UREAS, AS MODULATORS OF KINASE ACTIVITY - Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.11-11-2010
20100286189(AZA)INDOLE DERIVATIVE SUBSTITUTED IN POSITION 5, PHARMACEUTICAL COMPOSITION COMPRISING IT, INTERMEDIATE COMPOUNDS AND PREPARATION PROCESS THEREFOR - An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.11-11-2010
20120302597NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.11-29-2012
20120302596AZAINDOLES HAVING SEROTONIN RECEPTOR AFFINITY - Described herein are compounds with affinity for the 5-HT11-29-2012
20100324081PREVENTIVE, INHIBITOR OR REMEDY FOR CEREBRAL ANEURYSM COMPRISING IBUDILAST AS AN ACTIVE INGREDIENT - Herein provided is an agent for the prevention of cerebral aneurysm, for the control of the formation thereof or for the treatment thereof, which comprises Ibudilast as an effective component.12-23-2010
20100324083Combinations of Organic Compounds - The invention provides a pharmaceutical combination comprising: 12-23-2010
20100324082ENANTIOMERIC COMPOSITIONS OF 2-AMINO-1-(2-ISOPROPYLPYRAZOLO[1,5-a]PYRIDIN-3-YL)PROPAN-1-ONE AND RELATED METHODS - Enantiomerically pure (S)-2-amino-1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one, (S)-AV1013, is a candidate therapeutic for treating neuroathic pain, addiction behavior and drug withdrawal symptoms. Also described are methods for preparing and using (S)-AV1013, its pharmaceutically acceptable salts as well as pharmaceutically acceptable formulations of the same.12-23-2010
20110152311NOVEL CRYSTALLINE FORMS OF TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE SODIUM SALT - The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.06-23-2011
200901768247- (4-substituted-3-cyclopropylaminomethyl-1-pyrrolidinyl) quinolonecarboxylic acid derivative technical field - Object To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents. 07-09-2009
20090239897NOVEL COMPOUNDS - Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.09-24-2009
20100190819alpha-7 Nicotinic Acetylcholine Receptor Allosteric Modulators, Their Derivatives and Uses Thereof - The present application is related to compounds represented by Formula I, which are novel allosteric modulators of α7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on α7nAChR in a mammal by administering an effective amount of a compound of Formula I.07-29-2010
20110136857PYRROLE[2,3-B]PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS - Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.06-09-2011
20110136856Novel imidazo[1,5-a]pyridine derivatives, method for preparing same and pharmaceutical compositions containing same - The invention concerns compounds of formula I, a method for preparing said compounds, pharmaceutical compositions containing same and the theraprutic uses thereof.06-09-2011
20110190334Heterocyclic Sulfonamide Derivatives - The present invention relates to compounds of Formula I08-04-2011
20110201642Bioactive Compounds - The invention relates to bioactive compounds derived from an endophytic 08-18-2011
20100022581PYRROLIDINE-SUBSTITUTED AZAINDOLE COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT01-28-2010
20110218214Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme - The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.09-08-2011
20100267762NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.10-21-2010
20100125086USE OF ISOQC INHIBITORS - The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.05-20-2010
20090291977Chromane Derivatives Useful As Acid Pump Antagonists - This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R′, R11-26-2009
20080306105DEUTERIUM-ENRICHED MOXIFLOXACIN - The present application describes deuterium-enriched moxifloxacin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.12-11-2008
20100048609PHARMACEUTICAL DOSAGE FORMS FOR (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OX- O-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID - Provided herein are light protective pharmaceutical packages for enantiomerically pme (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid. In certain embodiments, the pharmaceutical packages comprise a glass vial containing SNS-595 drug product within a secondary container.02-25-2010
20110039880ARYL SUBSTITUTED SULFONAMIDE COMPOUNDS AND THEIR USE AS ANTICANCER AGENTS - Aryl substituted sulfonamide compounds of formula (I):02-17-2011
20120178776DIHYDRONAPHTHYRIDINYL(ORGANO)METHANONE ANALOGS AS POSITIVE ALLOSTERIC MGLUR5 MODULATORS - In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.07-12-2012
20090111847PREPARATION METHOD AND USE OF COMPOUNDS HAVING HIGH INSECTICIDAL ACTIVITIES - The present invention discloses a kind of nitromethylene derivatives as well as their preparation method and their uses. The insecticidal activity tests show that the nitromethylene derivatives of the present invention not only show high insecticidal activities against insects with piercing-sucking type or scratching type mouthparts, such as aphid, leafhopper, plant hopper, thrips and white fly and their resistant strains, but also show high insecticidal activities against 04-30-2009
20080234313NOVEL INHIBITORS - Compounds of formula (I), combinations and uses thereof for disease therapy,09-25-2008
201002677617-Azaindole Derivatives as Selective 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors - The present invention relates to 7-azaindole derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.10-21-2010
20100010035Novel Dual Action Receptors Antagonists (Dara) at the Ati and Eta Receptors - The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.01-14-2010
201101661733,5-DISUBSTUTUTED 1H-PYRROLO [2,3-B] PYRIDINES AS JNK INHIBITORS - The present invention provides novel compounds of forumula (I) and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.07-07-2011
201101661757-AZAINDOLE DERIVATIVES - Novel 7-azaindole derivatives of the formula (I), in which U, L, R, Y, X07-07-2011
20110166174COMPOUNDS MODULATING C-KIT AND C-FMS ACTIVITY AND USES THEREFOR - Compounds active on the receptor protein tyrosine kinases c-kit and c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or condition and c-fms-mediated diseases or condition, and methods for the use thereof.07-07-2011
20120015975FUSED HETEROCYCLIC COMPOUND AND USE THEREOF - A fused heterocyclic compound of formula (1): wherein, A01-19-2012
20120015973MEK MUTATIONS CONFERRING RESISTANCE TO MEK INHIBITORS - The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of MEK. In particular embodiments, the invention concerns mutations in a MEK sequence that confer resistance to a MEK inhibitor. Identification of such mutations in a MEK sequence allows the identification and design of second-generation MEK inhibitors. Methods and kits for detecting the presence of a mutant MEK sequence in a sample are also provided.01-19-2012
20120015974IMIDAZOPYRIDINE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I:01-19-2012
20090239898FURTHER THERAPEUTIC USE OF ZOLPIDEM - An imidazo[1,2-a] pyridine-3-acetamide such as zolpidem is useful in the treatment of a condition of the brain which has a lesion and exhibits diaschisis/dormant cells at the contralateral and other sites, more particularly trauma-induced injury, spinocerebellar ataxia, cerebellar or cerebral infarct and Ramsey-Hunt syndrome.09-24-2009
20120022098COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.01-26-2012
20120065224PYRROLO[3,2-C) PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF - The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect.03-15-2012
20110092538COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.04-21-2011
201100925372,6-Diaminopyridine Compounds Suitable For Treating Diseases Associated With Amyloid Or Amyloid-Like Proteins Or For Treating Or Preventing Ocular Diseases Or Conditions Associated With A Pathological Abnormality/Change In The Tissue Of The Visual System - The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.04-21-2011
20110092536NOVEL ANTI-INFECTIOUS DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME AND USES OF SAID DERIVATIVES IN TREATMENT - The invention relates to bi-substrate inhibitor molecules associating (i) a pyridine, pyridinium or dihydropyridine-type structure allied to active metabolites of isoniazide, or related structures, and (ii) a hydrophobic substituent. The invention also relates to the method for producing said molecules, to the pharmaceutical compositions containing said molecules, and to the use thereof as inhibitors of enoyl reductase for the preparation of a medicament, especially an anti-infectious medicament for the treatment of tuberculosis.04-21-2011
20120115900SUBSTITUTED NAPHTHYRIDINE DERIVATIVES AND THEIR MEDICAL USE - The present application discloses novel substituted naphthyridine derivatives of Formula (I) and their use as modulators of the voltage gated K05-10-2012
20110065745POLYSUBSTITUTED 2-ARYL-6-PHENYLIMIDAZO[1,2-A]PYRIDINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I):03-17-2011
20120283287CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS - Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.11-08-2012
20120316194APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula12-13-2012
20110184013Imidazo[1,2-a]Pyridine Compounds As Receptor Tyrosine Kinase Inhibitors - Compounds of Formula I and II: I II having the chemical names cis-6-fluoro-8-(3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline and 6-fluoro-8-(trans-3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline, respectively, and enantiomers and pharmaceutically acceptable salts thereof, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. The compounds of this invention have also been found to be inhibitors of Pim-1.07-28-2011
20110184012METHODS AND COMPOSITIONS FOR ALLEVIATING STUTTERING - Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor modulators. Active enantiomers, active metabolites, and pharmaceutically acceptable salts of garnma-aminobutyric acid receptor modulators, including cyclopyrrolones, are acceptable components of the compositions. The cyclopyrrolone class of modulators includes pagoclone, suriclone, zopiclone, 2-(7-chloro-2-naphthyridin-1,8-yl)-3-(5-methyl-2-oxohexy))isoindolin-1-one, 2-(7-chloro-2-naphthyridin-1,8-yl)isoindolin-1-yl-4- acetamidobutyrate, and 2-(7-chloro-1,8-naphthyridin-2y1)-3-(5-methyl-5-hydroxy-2-oxohexyl)-1-isoindolinone.07-28-2011
20120165366COMPOUNDS AND USES THEREOF - N-[3-(4-Cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, N-[3-(4-ethynyl-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including pain and polycystic kidney disease.06-28-2012
20120129884PHOTOCHEMOTHERAPEUTIC HETEROCYCLIC AGENTS HAVING ANTIPROLIFERATIVE AND ANTINEOPLASTIC ACTIVITY - The present invention concerns the synthesis of new analogs of angelicins, pyrrolo [3,2-h]quinoline, for the treatment of pathologies having hyperproliferative character included those having neoplastic nature. The treatment is based on the combined action of pyrrolo [3,2-h]quinolines and UV-A light, through a clinical approach defined as PUVA (psoralen-UVA light). The most important feature of these compounds is that they exert their remarkable photoxicity without any DNA damage, which is the main origin of the side effects of the PUVA therapy.05-24-2012
20120214840INDOLIZINE INHIBITORS OF 5-LIPOXYGENASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.08-23-2012
20120214839TREATMENT OF PROGRESSIVE NEURODEGENERATIVE DISEASE WITH IBUDILAST - Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).08-23-2012
20100197723BICYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME - Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.08-05-2010
20100173931HARMINE DERIVATIVES FOR REDUCING BODY WEIGHT - The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.07-08-2010
20100173930Certain Chemical Entities, Compositions and Methods - Provided are certain chemical entities, and methods of use to modulate diskeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, muscle spasm, neuromuscular disease, and other indications.07-08-2010
20120172390METHOD OF TREATING SLEEP DISORDERS USING THE COMBINATION OF EPLIVANSERIN AND ZOLPIDEM - The instant invention relates to a method of treating sleep disorders by using eplivanserin or pharmaceutically acceptable salts or esters thereof and Zolpidem by evaluating the effect of eplivanserin combined with the sleep-inducing agent Zolpidem on psychomotor/cognitive performance.07-05-2012
201000100371H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES USEFUL AS HSP90 INHIBITORS - Compounds of formula (I) have HSP90 inhibitory activity:01-14-2010
20100010038TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula01-14-2010
20120220622HETEROCYCLIC DERIVATIVES08-30-2012
20120258982ADAMANTYL COMPOUNDS - The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I:10-11-2012
20120190707SELECTIVE INHIBITORS OF AKT AND METHODS OF USING SAME - The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase. In general, the method comprises: (1) providing a plurality of compounds suspected of having Akt1 kinase inhibitory activity; (2) modeling the docking of each of the plurality of the compounds with a target binding site; (3) ranking the docked compounds by goodness of fit; (4) further selecting compounds; (5) optionally, visually analyzing structures of compounds selected in step (4) to remove any compounds with improbable docking geometry; and (6) experimentally testing the selected compounds from step (4) or step (5), if step (5) is performed, to determine their inhibitory activity against Akt1. The invention also encompasses pharmaceutical compositions including compounds whose inhibitory activity against Akt1 is discovered by the screening method, as well as methods of use of the pharmaceutical compositions to prevent and treat cancer and other conditions.07-26-2012
20090018156Pyrrolo [2,3,B] Pyridine Derivatives Useful As RAF Kinase Inhibitors - The present invention provides pyrrolo pyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.01-15-2009
20120232108GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I.09-13-2012
20120322820METHODS TO INHIBIT TUMOR CELL GROWTH BY USING PROTON PUMP INHIBITORS - Methods of treating one or more growth deregulated cells are disclosed. An effective amount of a pharmaceutical composition including a proton pump inhibitor is administered thereby treating a growth deregulated cell outside of the gastric lumen of a subject.12-20-2012
20120270897ACETYLENE DERIVATIVES OF 5-PHENYL-PYRAZOLOPYRIDINE, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF - Compounds of formula (I):10-25-2012
20120095034PIPERIDINE DERIVATIVES USEFUL AS OREXIN RECEPTOR ANTAGONISTS - This invention relates to imidazo[1,2-a]pyridin-2-ylmethyl substituted piperidine derivatives of formula (I) and their use as pharmaceuticals, in the treatment of obesity and diabetes.04-19-2012
20110224247AZAISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.09-15-2011
20100234418COMPOUNDS AND USES THEREOF - N-[3-(4-Cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, N-[3-(4-ethynyl-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-4-trifluoromethyl-benzenesulfonamide, and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including pain and polycystic kidney disease.09-16-2010
20120277263POLYMORPHS OF 1-CYCLOPROPYL-7-([S,S])-2,8-DIAZADICYCLO[4.3.0]NON-8-YL)-6-FLUORO-1,4-DIH- YDRO -8-METHOXY-4-OXO-3-QUINOLINE CARBOXYLIC ACID HYDROCHLORIDE AND METHODS FOR THE PREPARATION THEREOF - Two novel crystalline forms, designated form A and form B of the antibacterial agent 1-cyclopropyl-7-([S,S])-2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride of formula,11-01-2012
20120277261PHARMACEUTICAL FORMULATIONS USEFUL IN THE TREATMENT OF INSOMNIA - There is provided a formulation suitable for transmucosal administration comprising a short acting hypnotic drug, which formulation provides a measurable plasma concentration of drug within 10 minutes of administration. The formulation is capable of providing sleep on demand, and preferably comprises particles of drug, for example zolpidem or a pharmaceutically-acceptable salt thereof and a mucoadhesion promoting agent, such as sodium carboxymethylcellulose, which particles of drug and mucoadhesive are presented upon the surface of larger carrier particles.11-01-2012
200901494927,8-DIHYDRO-1,6-NAPHTHYRIDIN-5(6H)-ONES AND RELATED BICYCLIC COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an DPP4 modulated disease or disorder such as, for example, diabetes, by administration of a therapeutically effective dose of a compound according to Formula I.06-11-2009
20110263638Therapeutic agent for glaucoma comprising rho kinase inhibitor and - blocker - A therapeutic agent for glaucoma including a combination of pharmaceutically effective amounts of a Rho kinase inhibitor and a β-blocker, wherein the Rho kinase inhibitor is (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide and the β-blocker is befunolol, carteolol, nipradilol, betaxolol, levobunolol or metipranolol. A method of treating glaucoma including administering effective amounts of a Rho kinase inhibitor and a β-blocker to a patient, wherein the Rho kinase inhibitor is (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide and the β-blocker is befunolol, carteolol, nipradilol, betaxolol, levobunolol or metipranolol.10-27-2011
20100204266COMPOSITIONS FOR USE IN IDENTIFICATION OF MIXED POPULATIONS OF BIOAGENTS - The present invention provides oligonucleotide primers, compositions, and kits containing the same for rapid identification of bacterial bioagents and populations of bioagents which are members of the 08-12-2010
20100204265Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections - Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).08-12-2010
20120329826SUBSTITUTED-5-AMINOPYRROLO/PYRAZOLOPYRIDINES - Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by RON and/or MET.12-27-2012
201201011241,2,4-OXADIAZOL DERIVATIVES, THEIR PHARMACEUTICAL COMPOSITIONS AND THEIR USE AS SPHINGOSINE 1-PHOSPHATE 1 RECEPTOR AGONISTS - 1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed.04-26-2012
20120101123COMPOUNDS - The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.04-26-2012
20120101122IMIDAZO[1,2 A] PYRIDINE 6 CARBOXAMIDE DERIVATIVES, THEIR USE FOR THE TREATMENT OF COLON CANCER AND THEIR METHOD OF MANUFACTURE - This invention relates to the manufacture of novel chemical compounds which have biological activity, particularly to novel chemical compounds that are cytotoxic against colon cancer cells and colon cancer cell lines. The manufacturing of said chemical compounds displaying anti-cancer properties employs the use of multi-component chemical reactions. The object of this invention is to manufacture and isolate analogues of imidazo[1,2-a]pyridine, namely compounds of Formula 1, which are cytotoxic against colon cancer cells, while concomitantly being relatively inactive against white blood cells.04-26-2012
20100168155DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The present invention is related to a compound of formula (I):07-01-2010
20100130540AZAQUINOLINONE DERIVATIVES AND USES THEREOF - The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.05-27-2010
20130018070MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.01-17-2013
201300235545-PHENYLPYRAZOLOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I):01-24-2013
20080255183N-[HETEROARYLCARBONYL]-3-THIENYL-L-ALANINE DERIVATIVES AS a5beta1 ANTAGONISTS - The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to a5b1 antagonists that also exhibit appropriate selectivity profile(s) against other integrins.10-16-2008
200802491261,3-SUBSTITUTED CYCLOALKYL DERIVATIVES HAVING ACIDIC, MOSTLY HETEROCYCLIC GROUPS, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives.10-09-2008
200802278075-LIPOXYGENASE-ACTIVATING PROTEIN (FLAP) INHIBITORS - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.09-18-2008
20080227806Novel Drugs for Dementia - The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.09-18-2008
200802211524-(HETEROARYL-METHYL AND SUBSTITUTED HETEROARYL-METHYL)-IMIDAZOLE-2-THIONES ACTING AS ALPHA2 ADRENERGIC AGONISTS - Compounds of Formula 109-11-2008
200802211513-AMINO-2-PHENYLPYRROLIDINE DERIVATIVES - 3-amino-2-phenylpyrrolidine compounds useful as NK-1 antagonists, with pharmaceutical compositions and methods of treatment comprising same, are disclosed.09-11-2008
20080221150Prevention of Neurodegeneration by Macrolide Antibiotics - The present disclosure describes the use of macrolide antibiotics to prevent neurodegeneration and to treat or prevent disease and conditions which involve neurodegeneration. While not being limited to a specific mechanism of action, in one embodiment, the macrolide antibiotics inhibit neurodegeneration caused by lysosomal and/or mitochondrial dysfunction. The present disclosure contemplates the use of any macrolide antibiotic and pharmaceutically acceptable derivatives thereof. In a specific embodiment, the macrolide antibiotics include bafilomycin A1, bafilomycin B1 and concanamycin.09-11-2008
20080221148COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.09-11-2008
20130178496MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.07-11-2013
20130178495IBUDILAST FOR RELIEVING NEGATIVE EFFECTS OF MEDICATION OVERUSE HEADACHE - Certain negative effects of medication overuse headache (MOH) are relieved by administering ibudilast or a pharmaceutically acceptable salt thereof.07-11-2013
20080214598Novel Piperidine Carboxylic Acid Amide Derivatives - The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.09-04-2008
20130102628CRYSTAL OF FUSED PYRIDINE COMPOUND SALT - [Problem] A salt or crystal of a compound which is highly stable in a solid state and useful as a bulk material for the preparation of a pharmaceutical product is provided.04-25-2013
201301580664-AZAINDOLE INHIBITORS OF CRAC - Disclosed are compounds of Formula (I):06-20-2013
20130143910Fructose-1,6-biphosphatases as new targets for diagnosing and treating breast cancer brain metastasis - A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.06-06-2013
20130143911MEK1 Mutation Conferring Resistance to RAF and MEK Inhibitors - Nucleic acids and proteins having a mutant MEK sequence, and methods concerning identification of patients having resistance to treatment with anti-cancer agents, specifically inhibitors of RAF or MEK are provided. Methods of treatment and for optimizing treatment for patients having a mutation in a MEK1 sequence are also provided.06-06-2013
20130143913PROPHYLACTIC OR THERAPEUTIC AGENT FOR NON-ALCOHOLIC STEATOHEPATITIS - An object of the present invention is to provide an agent for prevention or treatment of a fatty liver disease, preferably NAFLD, more preferably NASH. The present invention provides an agent for prevention or treatment of a fatty liver disease containing ibudilast as an active agent.06-06-2013
20130158067TRPV1 Antagonists - Disclosed herein are compounds of formula (I):06-20-2013
20130158068DICARBOXIMIDE DERIVATIVES OF BERBAMINE, THE PREPARATION AND USE THEREOF - The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament.06-20-2013
20080280946Azaindole-Derivatives As Factor Xa Inhibitors - Indazole-derivatives as factor Xa inhibitors The present invention relates to compounds of the formula I11-13-2008
20080200496SUBSTITUTED 1H-PYRROLO[3,2-b, 3,2-c, and 2,3-c]PYRIDINE-2-CARBOXAMIDES AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE Ie - The present invention discloses and claims compounds of formula (I)08-21-2008
20080200495Pyrrolopyridine Compounds, Method of Making Them and Uses Thereof - Pyrrolopyridine compounds corresponding to formula (I):08-21-2008
20080200494Imidazopyridine Derivatives - The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R08-21-2008
20110212992NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.09-01-2011
20110224249Novel Hydrate Form - The present invention relates to a novel hydrate form of moxifloxacin monohydrochloride, processes for preparing the form, pharmaceutical compositions comprising the form and uses of the form and compositions.09-15-2011
20110275665GLUCOKINASE ACTIVATORS - Compounds are provided for use with hexokinases that comprise:11-10-2011
20110275664Method for treating drug and behavioral addictions - The present invention is directed to the use of ibudilast for treating addictions, including drug and behavioral addictions. In particular, ibudilast is used to diminish the dopamine-mediated reward associated with addictions and to treat withdrawal syndromes after discontinuance of addictive drug use or behavior. In addition, methods are provided for preventing or inhibiting relapse in human subjects having a history of methamphetamine addiction or dependence by the administration of an effective amount of ibudilast.11-10-2011
20110275663N-Acylthiourea and N-Acylurea Inhibitors of the Hedgehog Protein Signalling Pathway - The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.11-10-2011
20110237619IMIDAZOPYRIDINE DERIVATIVES WHICH INHIBIT THE SECRETION OF GASTRIC ACID - The present invention relates to substituted imidazo[1,2-a]pyridines of formula I where R is —CH09-29-2011
20120277262NEW AMINOTETRALINE DERIVATIVES - The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds in producing medicaments for the treatment of various diseases and conditions, such as of the central nervous system.11-01-2012
20130150400SALTS, PRODRUGS AND POLYMORPHS OF FAB I INHIBITORS - In part, the present invention is directed to antibacterial compounds and salts thereof.06-13-2013
20100076013Methods of Treatment - The present invention relates to methods of treating hematological malignancies, including acute myeloid leukemia (AML), comprising the use of compounds that inhibit the binding of the Smac protein to IAPs (“IAP inhibitor”). The present invention also relates to the use of IAP inhibitors for the preparation of a medicament to treat hematological malignancies, including AML.03-25-2010
201003176882-HETEROAROYLIMIDAZOL[1,2-a]PYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I):12-16-2010
201003176872-BENZOYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - Compounds of formula (I)12-16-2010
20100317686N-HETEROCYCLIC-6-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I):12-16-2010
20100317685N-PHENYL-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - Compounds of formula (I):12-16-2010
20130131102SELECTIVE GLYCOSIDASE INHIBITORS - The present invention provides glucoimidazole derivatives and methods of making them. The compounds can be used to inhibit the activity of O-GlcNAcase enzymes, including both bacterial OGA (bOGA) and human OGA (hOGA) and can be selective, showing low inhibition of hexosaminidases. The compounds can be used to study the role of the O-GlcNAcase modification in human or animal cells. Furthermore the compounds can have therapeutic uses in the treatment of diseases mediated by the activity of O-GlcNAcase enzymes including type II diabetes, Alzheimers Disease, and cancer.05-23-2013
20090306125Mitochondria-Targeted Antioxidant Prodrugs and Methods of Use - The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.12-10-2009
20110288117SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I):11-24-2011
20110288116IAP INHIBITORS - The present invention describes compounds of the following formula: processes for their preparation, pharmaceutical compositions containing them, and their use in therapy. The compounds of the present invention inhibit IAPs (inhibitors of apoptosis proteins) and thus are useful in the treatment of cancer, autoimmune diseases and other disorders where a defect in apoptosis is implicated.11-24-2011
20110312989INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.12-22-2011
20110312988SNS-595 AND METHODS OF USING THE SAME - The present invention relates to SNS-595 and methods of treating cancer using the same.12-22-2011
20110312987SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE - 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.12-22-2011
20110319443INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.12-29-2011
201302038023 -AMINO- PYRAZOLE DERIVATIVES USEFUL AGAINST TUBERCULOSIS - A compound of Formula (I) or a pharmaceutically acceptable salt thereof:08-08-2013

Patent applications in class Plural hetero atoms in the bicyclo ring system

Patent applications in all subclasses Plural hetero atoms in the bicyclo ring system